Synthetic biopolymers have been shown to exhibit physical and chemical properties that can be widely utilized for biologically therapeutic purposes. Amphiphilic block and random copolymers consisting poly(ethylene glycol) (PEG) and poly(amino acid) (PAA) segments allow for the construction of biomedically applicable delivery systems for both drug and gene therapies. Within PEG-PAA copolymers, PEG provides biocompatibility while PAAs permit tunable hydrophilic, ionic (cationic and anionic), and hydrophobic characteristics within the polymer constructs when using specific amino acid moieties. By using amino acids with ionic side chains, amphiphilicity and solubility of PEG-PAA copolymers can be regulated, allowing for nanoparticle formation with biologically active small molecules and plasmid DNA in aqueous solutions. PEGylated PAAs are synthesized using an amino-terminated PEG as the macroinitiator for ring opening polymerization of amino acid N-carboxyanhydrides. The self-assembly of block and random copolymers comprised of PEG and p(L-Glutamate) or p(L-Lysine) and p(L-Leucine) will be discussed. Due to cationic charge provided by p(L-Lys) blocks, PEGylated-p(L-Lysine)-p(L-Leucine) copolymers were examined for their capability of complexing with DNA and forming small polyplexes for gene transfections. Results such as dynamic light scattering, Dnase protection, and transfection will be discussed. PEGylated PAA copolymers containing p(L-Glutamate) and p(L-Leucine) were studied for their ability to properly encapsulate hydrophobic drugs, such as indomethacin and doxorubicin hydrochloride, and increased their solubility in aqueous systems.

Synthesis and utilization of cationic and anionic PEGylated poly(amino acid)s for gene and drug delivery

251st National Meeting (2016)

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